Enzalutamide and Cancer

Prostate carcinoma is androgen-dependent, and therefore the main target of treatment is lowering androgen levels. Medical or surgical castration, androgen receptor-blocking agents, androgen-synthesis inhibitors, chemotherapy, sipuleucel-T, and radium-223 are treatment options. Enzalutamide is a relatively new androgen-signaling inhibitor that has 5 to 8 times greater affinity for the androgen receptor (AR) than bicalutamide. Enzalutamide does not demonstrate agonistic activity on ARs. Enzalutamide induces apoptosis of prostate cancer cells. Enzalutamide is effective in metastatic castration-resistant prostate cancer in patients with progression after docetaxel treatment and in chemotherapy-naive patients. Enzalutamide is also superior to the commonly used AR blocking agent bicalutamide in chemotherapy-naive metastatic and non-metastatic castration-resistant prostate cancer patients. Its efficacy has been proven in hormone-naive patients, and several trials are ongoing. Enzalutamide has a favorable side effect profile and improves quality of life and pain scores.